- Unprecedented convergent synthesis of the fused tricyclic thiophenes via Friedel-Crafts cycliacylation reactions
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An efficient and concise procedure toward benzo-and pyridothieno[2,3-b] fused N-heterocycles from readily available substrates is described. The process involves Lewis and Bronsted acids-mediated Friedel-Crafts cyclizations of the synthesized thiophene-ba
- Abd El-Aal, Hassan A.K.,Khalaf, Ali A.
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- Substituted 2-Aminothiopen-derivatives: A potential new class of GluR6-Antagonists
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In the course of search for new therapeutic agents against epilepsy new inhibitors for the kainate receptor subtypes GluR5 and GluR6 were synthesized. We were able to synthesize new substituted thieno[2,3-d]pyrimidines 3a,b, 4a,b, 5a,b as well as thiophene-3-carboxamides 2a-d and a multitude of substituted 4-methyl-5-phenylthiophene-3-carboxylic acids. All compounds described herein were tested for their antagonistic effect towards the kainate receptor subtypes GluR5 and GluR6. The highest activity was observed for ethyl 2-amino-4-methyl-5-phenylthiophene-3-carboxylate 1c with an IC50 = 0.75 μM at the GluR6 receptor.
- Briel,Rybak,Kronbach,Unverferth
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experimental part
p. 69 - 77
(2010/03/24)
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- Processes for the production of thienopyrimidine derivatives
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The present invention provides a process for producing an intermediate for thienopyrimidine derivatives having the GnRH antagonistic activity at an industrial large scale. The process for production of the present invention relates to a process for produc
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- Thienopyridine derivatives, their intermediates and production thereof
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The present invention provides an intermediate for producing a thienopyridine derivative useful as a GnRH antagonist as well as an efficient and safe method for producing the same in an industrial scale at a high yield.
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- Thienopyrimidine derivatives, their production and use
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Thienopyrimidine derivatives are disclosed. Also disclosed are methods for the production and use of these compounds.
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- Prolactin production inhibitory agent
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The prolactin production inhibition agent of the present invention containing a condensed cyclic compound, which is characterized by containing a condensed bicyclic structure of an optionally substituted homo or hetero 5- to 7-membered ring with an optionally substituted homo or hetero 5- to 7-membered ring, or a salt thereof, can be used, as a medicine, for the prophylaxis or therapy of diseases accompanied with an excess prolactin production or diseases having enhanced reactivity with prolactin, or is useful for inhibiting puerperal lactation, and also useful as a prophylactic or therapeutic agent of galactorrhea, hyperprolactinemic ovulation disturbance, amenorrhea-galactorrhea syndrome, prolactinoma, and besides, interbrain tumor, and acromegaly, pituitary gigantism.
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- THIENOPYRIDINE COMPOUNDS WHICH HAVE USEFUL PHARMACEUTICAL ACTIVITY
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The present thienopyrimidine derivatives and compositions having gonadotropin-releasing hormone antagonistic activity are useful as propylactics or therapeutic agents for the prevention or treatment of several hormone dependent diseases, for example, a se
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- Thieno[2,3-d]pyrimidine-3-acetic acids a new class of nonpeptide endothelin receptor antagonists
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On the basis of structural information for the cyclic hexapeptide endothelin (ET) receptor antagonist, TAK-044, a series of thieno[2,3- d]pyrimidine-2,4-dione derivatives bearing a carboxyl group and aromatic rings that were important for receptor binding
- Cho, Nobuo,Nara, Yoshi,Harada, Mioko,Sugo, Tsukasa,Masuda, Yasushi,Abe, Akemi,Kusumoto, Keiji,Itoh, Yasuaki,Ohtaki, Tetsuya,Watanabe, Toshifumi,Furuya, Shuichi
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p. 1724 - 1737
(2007/10/03)
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- Method for the production of recombinant human LH-RH receptor proteins
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Disclosed are CHO cells which are capable of continued production of human LH-RH receptor proteins, or cell membrane fractions thereof; recombinant human LH-RH receptor proteins or partial peptides thereof; methods for screening compounds which have affinity for an LH-RH receptor by contacting the compound with the CHO cells or the cell membrane fractions thereof, or the recombinant human LH-RH receptor proteins or the partial peptides thereof; kits for screening them; the compounds which have affinity for the LH-RH receptor obtained by methods for the screening or kits for the screening; and pharmaceutical compositions containing the compound, thereby being able to early provide prophylactic or therapeutic compositions, for example, for prostate cancer, uterine cancer, breast cancer, a pituitary tumor, endometriosis, hysteromyoma or precocious puberty. They are also useful as a pregnancy controlling composition such as contraceptive or a menstrual cycle controlling composition.
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- Method of regulating the growth of plants
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Novel method for regulating the growth of plants which method comprises applying to the plants or their habitat, effective amounts of heterocyclic compound of the formula STR1 in which R1 is alkyl or optionally substituted aryl, R2 is hydrogen, alkyl or optionally substituted aryl, R3 is hydrogen or the radical STR2 in which Y is oxygen or sulfur and R5 is alkyl, haloalkyl, alkoxyalkyl, aryloxyalkyl, which is optionally substituted in the aryloxy part, alkoxy, optionally substituted aryl, optionally substituted aryloxy, monoalkylamino, dialkylamino, alkenylamino, dialkenylamino, optionally substituted arylamino, a 5-membered to 7-membered heterocyclic ring, bonded via nitrogen, or the radical STR3 in which R6 is hydrogen or alkyl and R7 is hydrogen or alkyl, or R6 and R7, together with the adjacent nitrogen atom, are a 5-membered to 7-membered heterocyclic ring, R4 is cyano or the grouping --COR8 in which R8 is alkoxy or amino, and X is oxygen or sulfur.
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